Tris-azaaromatic quaternary ammonium salts: Novel templates as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.
Bioorg Med Chem Lett
; 17(24): 6701-6, 2007 Dec 15.
Article
in En
| MEDLINE
| ID: mdl-17977723
ABSTRACT
A series of tris-azaaromatic quaternary ammonium salts has been synthesized and evaluated for their ability to inhibit neuronal nicotinic acetylcholine receptors (nAChRs) mediating nicotine-evoked [(3)H]dopamine release from superfused rat striatal slices and for inhibition of [(3)H]nicotine and [(3)H]methyllycaconitine binding to whole rat brain membranes. The 3-picolinium compound 1,3,5-tri-{5-[1-(3-picolinium)]-pent-1-ynyl}benzene tribromide (tPy3PiB), 3b, exhibited high potency and selectivity for nAChR subtypes mediating nicotine-evoked [(3)H]dopamine release with an IC(50) of 0.2 nM and I(max) of 67%.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Aza Compounds
/
Receptors, Nicotinic
/
Nicotinic Antagonists
/
Quaternary Ammonium Compounds
/
Nicotine
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2007
Document type:
Article
Affiliation country:
United States